Cholinergics Flashcards
Nicotinic receptors have what structure and are what type of receptor?
Pentameric structure
Ligand-gated ion channels
What are the major muscarinic subtypes in the body?
M1, M3, M5 inositol phosphate pathway
M2, M4 inhibit adenylyl cyclase (reduce cAMP)
M1
CNS
Stomach
M2
Cardiac muscle
CNS
Airway smooth muscle
M3
Airway smooth muscle
Glandular smooth tissue
M4/5
CNS
Probably other stuff people will figure in the future, be thankful we’re taking this class now..
Nm
Skeletal muscle at NMJ
Nn
Autonomic ganglia
Adrenal medulla
CNS
Scopolamine and Atropine are ______ amines
Tertiary
Glycopyrrolate is _____ amine
Quaternary
Which antimuscarinic has the strongest antisialagogue and sedative effects?
Scopolamine
Which antimuscarinic has the strongest effect on increasing HR?
Atropine
Why is glycopyrrolate prefered over atropine in many cases?
Does not cross the BBB and thus has fewer CNS effects (little sedation)
Glycopyrrolate vs Atropine kinetics
IV atropine onset is 1 minute, duration 30-60 minutes. E1/2 2.3 hrs. 18% unchanged in urine, rest is hydrolyzed.
IV glycopyrrolate onset is 2-3 minutes, duration 30-60 minutes, E1/2 1.25 hrs, 80% unchanged in urine.
Who would see a bigger effect from atropine, an old patient or a young patient?
Young patient- high baseline vagal tone, this decreases as we age
What must we always give when antagonizing NMB?
Anticholinesterase drug
Ipratropium uses and dosing
Bronchodilation
MDI 40-80mcg 2 puffs
0.25-0.5mg via neb
30-90 minute onset time
Useful in asthmatics, COPD, and smokers prior to airway instrumentation
We would want to avoid anticholinergics in what type of ophtho cases?
Narrow angle glaucoma, it increase IOP
Anticholinergics can reduce what side effect of opioids?
Biliary and ureteral spasm
Scopolamine dosing
- 3-0.5mg or 5mcg/kg (pre-op)
1. 5mg transdermal (5mcg/hr x 72 hrs- nausea)
Atropine
0.2-0.4mg IV (pre-op)
0.4-1.0mg IV (bradycardia)
2mg in 5ml NS via neb (bronchodilation)
Glycopyrrolate
0.1mg-0.2mg IV (pre-op and bradycardia)
Central anticholinergic syndrome is more likely to occur with ________ and __________. What are the S/S and treatment?
Scopolamine and atropine
Restlessness, hallucinations, somnolence, unconsciousness
Delayed emergence/recovery in PACU
Give physostigmine 15-60 mcg/kg IV as needed q1-2 hours
Atropine doses below 0.4mg for bradycardia can actually do what?
Make the bradycardia worse!
Other anticholinergics
Ipratropium (Atrovent), Tiotropium (Spiriva)- COPD
Oxybutynin (Ditropan), Tolterodine (Detrol)- overactive bladder (M non-specific)
Darifenacin (Enablex), Solifenacin (Vesicare)- overactive bladder (M3 specific)
